Home Epigenetics Epigenetic Reader Domain inhibitor - Histone Methyltransferase inhibitor - PROTAC inhibitor UNC6852

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UNC6852 Epigenetic Reader Domain inhibitor

Cat.No.S9659

UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. This compound is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.
UNC6852 Epigenetic Reader Domain inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 832.97

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Quality Control

Batch: S965901 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.83%
99.83

Chemical Information, Storage & Stability

Molecular Weight 832.97 Formula
C43H48N10O6S
 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2688842-08-0 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(SC=N1)C2=CC=C(CNC(=O)C3CC(O)CN3C(=O)C(NC(=O)CCCNC(=O)C4=CC=C(C=C4)C5=CN=C(NCC6=CC=CO6)[N]7C=NN=C57)C(C)(C)C)C=C2

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (120.05 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
EED [1]
(Cell-free assay)
247 nM
In vitro

UNC6852 contains an EED226-derived ligand and a ligand for VHL which bind to the WD40 aromatic cage of EED and CRL2VHL, respectively, to induce proteasomal degradation of PRC2 components, EED, EZH2, and SUZ12. Degradation of PRC2 with this compound blocks the histone methyltransferase activity of EZH2, decreasing H3K27me3 levels in HeLa cells and diffuse large B cell lymphoma (DLBCL) cells containing EZH2 gain-of-function mutations. This chemical degrades both wild-type and mutant EZH2, and additionally displays anti-proliferative effects in this cancer model system.[1]
References

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